eplerenone (Rx)

Brand and Other Names:Inspra
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg

Hypertension (HTN)

Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day

Heart Failure Post MI

Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated

Dose adjustments may be required based on potassium levels

Renal Impairment

Contraindicated if CrCl <50 mL/min or serum creatinine >2 mg/dL in males or >1.8 mg/dL in females

Hepatic Impairment

Dose adjustment not necessary

Dosing considerations

In post-MI CHF patients taking a moderate CYP3A inhibitor, do not exceed 25 mg once daily; in patients with hypertension taking a moderate CYP3A inhibitor, initiate at 25 mg once daily; for inadequate blood pressure response, dosing may be increased to a maximum of 25 mg twice daily

Other Indications and Uses

Improving survival of stable patients with LV systolic dysfunction (LVEF ≤40%) and CHF after an acute myocardial infarction (MI)

Safety and efficacy not established

Hypertension

Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day

Heart Failure Post MI

Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated

Dose adjustments may be required based on potassium levels

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Interactions

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            Adverse Effects

            1-10%

            Hyperkalemia (2-10%)

            Increased risk of hyperkalemia with presence of renal dysfunction

            1-3%

            • Dizziness
            • Fatigue/malaise
            • Abdominal pain
            • Diarrhea
            • Albuminuria
            • Hypercholesterolemia
            • Hypertriglyceridemia
            • Cough

            <1%

            Abnormal vaginal bleeding

            Gynecomastia

            Mastodynia

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            Warnings

            Contraindications

            Hypersensitivity

            For all patients: Serum potassium >5.5 mEq/L at initiation Creatinine clearance ≤30 mL/min Concomitant use with strong CYP3A inhibitors For the treatment of hypertension: Type 2 diabetes with microalbuminuria Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females Creatinine clearance <50 mL/min Concomitant use of potassium supplements or potassium-sparing diuretics

            For all patients

            • Serum potassium >5.5 mEq/L at initiation
            • Creatinine clearance ≤30 mL/min
            • Concomitant use with strong CYP3A inhibitors

            For the treatment of hypertension

            • Type 2 diabetes with microalbuminuria
            • Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females
            • Creatinine clearance <50 mL/min
            • Concomitant use of potassium supplements or potassium-sparing diuretics

            Cautions

            Hyperkalemia, liver dysfunction, metabolic or respiratory acidosis, renal impairment, hypersensitivity to spironolactone

            The risk of hyperkalemia is higher in patients with impaired renal function, proteinuria , diabetes and those concomitantly treated with ACEs, ARBs, NSAIDs and moderate CYP3A inhibitors

            Patients taking moderate CYP3A inhibitors that cannot be avoided should have their dose of eplerenone reduced

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            Pregnancy & Lactation

            Pregnancy

            Available data from published case reports on eplerenone use during pregnancy are insufficient to establish a drug-associated risk of major birth defects, miscarriage, adverse maternal or fetal outcomes; in animal studies, no adverse developmental effects were observed when eplerenone was administered to pregnant rats and rabbits during organogenesis at exposures 32 and 31 times, respectively the human exposure at the 100 mg/day therapeutic dose

            Hypertension in pregnancy increases maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage); hypertension increases fetal risk for intrauterine growth restriction and intrauterine death; pregnant women with hypertension should be carefully monitored and managed accordingly

            Infertility

            • Based on animal data, therapy may compromise male fertility; in mature rates, male fertility was decreased with eplerenone exposure at 17 times the 100 mg/day human therapeutic dose; reversibility of effect, not evaluated

            Lactation

            There are no human data available on whether eplerenone is present in human milk, or has effects on breastfed infants or on milk production; eplerenone was present in milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Selective aldosterone receptor antagonist; blocks aldosterone binding at the mineralocorticoid receptor

            Pharmacokinetics

            Half-Life: 3.5-6 hr

            Peak Plasma Time: 1-2 hr

            Bioavailability: 69%

            Protein Bound: 50%

            Vd: 43-90 L

            Metabolism: primarily hepatic CYP3A4

            Metabolite: no active mets identified

            Total Body Clearance: 10 L/hr

            Excretion: feces (32%) and urine (67%)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            eplerenone oral
            -
            25 mg tablet
            eplerenone oral
            -
            50 mg tablet
            eplerenone oral
            -
            25 mg tablet
            eplerenone oral
            -
            50 mg tablet
            eplerenone oral
            -
            25 mg tablet
            eplerenone oral
            -
            50 mg tablet
            eplerenone oral
            -
            25 mg tablet
            eplerenone oral
            -
            50 mg tablet
            Inspra oral
            -
            50 mg tablet
            Inspra oral
            -
            25 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            eplerenone oral

            EPLERENONE - ORAL

            (eh-PLER-en-own)

            COMMON BRAND NAME(S): Inspra

            USES: This medication is used alone or in combination with other medicines to treat high blood pressure. It works by blocking a chemical (aldosterone) in your body which in turn lowers the amount of sodium and water the body retains. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems. It is also used to treat congestive heart failure following a heart attack.

            HOW TO USE: Take this medication by mouth, usually once or twice daily, with or without food, or as directed by your doctor. Use this medication regularly in order to get the most benefit from it. Remember to use it at the same time(s) each day.The dosage is based on your medical condition (high blood pressure, heart failure), response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).It may take up to 4 weeks for this medication to fully affect your blood pressure.Keep taking this medication even if you feel well. Most people with high blood pressure do not feel sick.

            SIDE EFFECTS: Headache, dizziness, diarrhea, or vomiting may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: abnormal vaginal bleeding, enlarged or sore breasts in males, symptoms of a high potassium blood level (such as muscle weakness, slow/irregular heartbeat).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking eplerenone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: high potassium blood levels (hyperkalemia), kidney disease, diabetes.This medication may increase your potassium levels. Before using potassium supplements or salt substitutes that contain potassium, consult your doctor or pharmacist.This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the effects of this drug, especially the raising of potassium blood levels.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also Precautions section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some of the products that may interact with this drug include: drugs that may increase the level of potassium in the blood (such as birth control pills containing drospirenone, potassium sparing "water pills" such as amiloride/spironolactone/triamterene), lithium.Other medications can affect the removal of eplerenone from your body, which may affect how eplerenone works. Examples include adagrasib, certain azole antifungals (such as ketoconazole, itraconazole), clarithromycin, cobicistat, nefazodone, certain HIV protease inhibitors (such as nelfinavir), ritonavir, St. John's wort, telithromycin, among others.Some products have ingredients that could raise your blood pressure or worsen your heart failure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe dizziness, severe muscle weakness, or irregular heartbeat.

            NOTES: Do not share this medication with others.Lifestyle changes that may help this medication work better include exercising, stopping smoking, and eating a low-cholesterol/low-fat diet. Consult your doctor for more details.Lab and/or medical tests (such as potassium blood levels, kidney function) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.Have your blood pressure checked regularly while taking this medication. Learn how to monitor your own blood pressure at home, and share the results with your doctor.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised December 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.